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1.
Sci Rep ; 14(1): 10244, 2024 05 03.
Artículo en Inglés | MEDLINE | ID: mdl-38702350

RESUMEN

Access to Hepatis C treatment in Sub-Saharan Africa is a clinical, public health and ethical concern. The multi-country open-label trial TAC ANRS 12311 allowed assessing the feasibility, safety, efficacy of a specific care model of HCV treatment and retreatment in patients with hepatitis C in Sub Saharan Africa. Between November 2015 and March 2017, with follow-up until mid 2019, treatment-naïve patients with HCV without decompensated cirrhosis or liver cancer were recruited to receive 12 week-treatment with either sofosbuvir + ribavirin (HCV genotype 2) or sofosbuvir + ledipasvir (genotype 1 or 4) and retreatment with sofosbuvir + velpatasvir + voxilaprevir in case of virological failure. The primary outcome was sustained virological response at 12 weeks after end of treatment (SVR12). Secondary outcomes included treatment adherence, safety and SVR12 in patients who were retreated due to non-response to first-line treatment. The model of care relied on both viral load assessment and educational sessions to increase patient awareness, adherence and health literacy. The study recruited 120 participants, 36 HIV-co-infected, and 14 cirrhotic. Only one patient discontinued treatment because of return to home country. Neither death nor severe adverse event occurred. SVR12 was reached in 107 patients (89%): (90%) in genotype 1 or 2, and 88% in GT-4. All retreated patients (n = 13) reached SVR12. HCV treatment is highly acceptable, safe and effective under this model of care. Implementation research is now needed to scale up point-of-care HCV testing and SVR assessment, along with community involvement in patient education, to achieve HCV elimination in Sub-Saharan Africa.


Asunto(s)
Antivirales , Bencimidazoles , Benzopiranos , Ciclopropanos , Hepacivirus , Compuestos Heterocíclicos de 4 o más Anillos , Lactamas Macrocíclicas , Leucina/análogos & derivados , Prolina/análogos & derivados , Quinoxalinas , Ribavirina , Sofosbuvir , Humanos , Sofosbuvir/uso terapéutico , Sofosbuvir/efectos adversos , Femenino , Masculino , Antivirales/uso terapéutico , Antivirales/efectos adversos , Ribavirina/uso terapéutico , Ribavirina/efectos adversos , Persona de Mediana Edad , Compuestos Heterocíclicos de 4 o más Anillos/uso terapéutico , Compuestos Heterocíclicos de 4 o más Anillos/efectos adversos , Bencimidazoles/uso terapéutico , Bencimidazoles/efectos adversos , Hepacivirus/genética , Hepacivirus/efectos de los fármacos , Adulto , Ciclopropanos/uso terapéutico , Ciclopropanos/efectos adversos , Estudios de Factibilidad , Carbamatos/uso terapéutico , Quimioterapia Combinada , África Occidental , África Central , Fluorenos/uso terapéutico , Fluorenos/efectos adversos , Respuesta Virológica Sostenida , Sulfonamidas/uso terapéutico , Sulfonamidas/efectos adversos , Resultado del Tratamiento , Prolina/uso terapéutico , Hepatitis C/tratamiento farmacológico , Ácidos Aminoisobutíricos , Hepatitis C Crónica/tratamiento farmacológico , Hepatitis C Crónica/virología , Genotipo
2.
PeerJ ; 12: e17360, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38737746

RESUMEN

Breast cancer is the most common invasive neoplasm and the leading cause of cancer death in women worldwide. The main cause of mortality in cancer patients is invasion and metastasis, where the epithelial-mesenchymal transition (EMT) is a crucial player in these processes. Pharmacological therapy has plants as its primary source, including isoflavonoids. Brazilin is an isoflavonoid isolated from Haematoxilum brasiletto that has shown antiproliferative activity in several cancer cell lines. In this study, we evaluated the effect of Brazilin on canonical markers of EMT such as E-cadherin, vimentin, Twist, and matrix metalloproteases (MMPs). By Western blot, we evaluated E-cadherin, vimentin, and Twist expression and the subcellular localization by immunofluorescence. Using gelatin zymography, we determined the levels of secretion of MMPs. We used Transwell chambers coated with matrigel to determine the in vitro invasion of breast cancer cells treated with Brazilin. Interestingly, our results show that Brazilin increases 50% in E-cadherin expression and decreases 50% in vimentin and Twist expression, MMPs, and cell invasion in triple-negative breast cancer (TNBC) MDA-MB-231 and to a lesser extend in MCF7 ER+ breast cancer cells. Together, these findings position Brazilin as a new molecule with great potential for use as complementary or alternative treatment in breast cancer therapy in the future.


Asunto(s)
Benzopiranos , Neoplasias de la Mama , Cadherinas , Transición Epitelial-Mesenquimal , Proteína 1 Relacionada con Twist , Vimentina , Humanos , Transición Epitelial-Mesenquimal/efectos de los fármacos , Femenino , Cadherinas/metabolismo , Vimentina/metabolismo , Vimentina/genética , Línea Celular Tumoral , Proteína 1 Relacionada con Twist/metabolismo , Proteína 1 Relacionada con Twist/genética , Benzopiranos/farmacología , Neoplasias de la Mama/patología , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/genética , Neoplasias de la Mama Triple Negativas/patología , Neoplasias de la Mama Triple Negativas/tratamiento farmacológico , Neoplasias de la Mama Triple Negativas/metabolismo , Neoplasias de la Mama Triple Negativas/genética , Células MCF-7 , Biomarcadores de Tumor/metabolismo , Biomarcadores de Tumor/genética , Invasividad Neoplásica/genética , Metaloproteinasas de la Matriz/metabolismo , Metaloproteinasas de la Matriz/genética , Proteínas Nucleares
3.
Bioresour Technol ; 401: 130708, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38636878

RESUMEN

In this study, the biochemical response of Phaeodactylum tricornutum to varying concentrations of inorganic selenium (Se) was investigated. It was observed that, when combined with fulvic acid, P. tricornutum exhibited enhanced uptake and biotransformation of inorganic Se, as well as increased microalgal lipid biosynthesis. Notably, when subjected to moderate (5 and 10 mg/L) and high (20 and 40 mg/L) concentrations of selenite under fulvic acid treatment, there was a discernible redirection of carbon flux towards lipogenesis and protein biosynthesis from carbohydrates. In addition, the key parameters of microalgae-based biofuels aligned with the necessary criteria outlined in biofuel regulations. Furthermore, the Se removal capabilities of P. tricornutum, assisted by fulvic acid, were coupled with the accumulation of substantial amounts of organic Se, specifically SeCys. These findings present a viable and successful approach to establish a microalgae-based system for Se uptake and biotransformation.


Asunto(s)
Benzopiranos , Biocombustibles , Biotransformación , Diatomeas , Diatomeas/metabolismo , Benzopiranos/metabolismo , Ácido Selenioso/metabolismo , Microalgas/metabolismo
4.
Mar Pollut Bull ; 202: 116353, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38598929

RESUMEN

Galaxolide (HHCB) and tonalide (AHTN) are dominant musks added to personal care products. However, the accumulate and trophic transfer of SMs through the marine food chain are unclear. In this study, organisms were collected from three bays in Bohai Sea to investigate the bioaccumulation, trophic transfer, and health risk of SMs. The HHCB and AHTN concentrations in the muscles range from 2.75 to 365.40 µg/g lw and 1.04-4.94 µg/g lw, respectively. The median HHCB concentrations in muscles were the highest in Bohai Bay, followed by Laizhou Bay and Liaodong Bay, consistent with the HHCB concentrations in sediments. The different fish tissues from Bohai Bay were analyzed, and the HHCB and AHTN concentrations followed the heart > liver > gill > muscles. The trophic magnification factors (TMF) were lower than 1 and the health risk assessment showed no adverse health effects. The results provide insights into the bioaccumulation and trophic transfer behavior of SMs in marine environments.


Asunto(s)
Monitoreo del Ambiente , Peces , Cadena Alimentaria , Contaminantes Químicos del Agua , Medición de Riesgo , Contaminantes Químicos del Agua/análisis , Contaminantes Químicos del Agua/metabolismo , Animales , Peces/metabolismo , China , Bioacumulación , Benzopiranos , Ácidos Grasos Monoinsaturados/análisis , Ácidos Grasos Monoinsaturados/metabolismo , Tetrahidronaftalenos/análisis , Bahías
5.
J Hazard Mater ; 470: 134304, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38615650

RESUMEN

In lightly polluted water containing heavy metals, organic matter, and green microalgae, the molecular weight of organic matter may influence both the growth of green microalgae and the concentration of heavy metals. This study elucidates the effects and mechanisms by which different molecular weight fractions of fulvic acid (FA), a model dissolved organic matter component, facilitate the bioaccumulation of hexavalent chromium (Cr(VI)) in a typical green alga, Chlorella vulgaris. Findings show that the addition of FA fractions with molecular weights greater than 10 kDa significantly enhances the enrichment of total chromium and Cr(VI) in algal cells, reaching 21.58%-31.09 % and 16.17 %-22.63 %, respectively. Conversely, the efficiency of chromium enrichment in algal cells was found to decrease with decreasing molecular weight of FA. FA molecular weight within the range of 0.22 µm-30 kDa facilitated chromium enrichment primarily through the algal organic matter (AOM) pathway, with minor contributions from the algal cell proliferation and extracellular polymeric substances (EPS) pathways. However, with decreasing FA molecular weight, the AOM and EPS pathways become less prominent, whereas the algal cell proliferation pathway becomes dominant. These findings provide new insights into the mechanism of chromium enrichment in green algae enhanced by medium molecular weight FA.


Asunto(s)
Benzopiranos , Chlorella vulgaris , Cromo , Microalgas , Peso Molecular , Contaminantes Químicos del Agua , Cromo/metabolismo , Cromo/química , Chlorella vulgaris/metabolismo , Chlorella vulgaris/crecimiento & desarrollo , Chlorella vulgaris/efectos de los fármacos , Contaminantes Químicos del Agua/metabolismo , Microalgas/metabolismo , Microalgas/efectos de los fármacos , Microalgas/crecimiento & desarrollo , Benzopiranos/química , Benzopiranos/metabolismo
6.
J Hazard Mater ; 470: 134244, 2024 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-38598879

RESUMEN

Spirulina platensis can secrete extracellular polymeric substances (EPS) helping to protect damage from stress environment, such as cadmium (Cd2+) exposure. However, the responding mechanism of S. platensis and the secreted EPS to exposure of Cd2+ is still unclear. This research focuses on the effects of Cd2+ on the composition and structure of the EPS and the response mechanism of EPS secretion from S. platensis for Cd2+ exposure. S. platensis can produce 261.37 mg·g-1 EPS when exposing to 20 mg·L-1 CdCl2, which was 2.5 times higher than the control group. The S. platensis EPS with and without Cd2+ treatment presented similar and stable irregularly fibrous structure. The monosaccharides composition of EPS in Cd2+ treated group are similar with control group but with different monosaccharides molar ratios, especially for Rha, Gal, Glc and Glc-UA. And the Cd2+ treatment resulted in a remarkable decline of humic acid and fulvic acid content. The antioxidant ability of S. platensis EPS increased significantly when exposed to 20 mg·L-1 CdCl2, which could be helpful for S. platensis protecting damage from high concentration of Cd2+. The transcriptome analysis showed that sulfur related metabolic pathways were up-regulated significantly, which promoted the synthesis of sulfur-containing amino acids and the secretion of large amounts of EPS.


Asunto(s)
Cadmio , Spirulina , Spirulina/efectos de los fármacos , Spirulina/metabolismo , Cadmio/toxicidad , Sustancias Húmicas , Matriz Extracelular de Sustancias Poliméricas/metabolismo , Matriz Extracelular de Sustancias Poliméricas/efectos de los fármacos , Benzopiranos/farmacología , Antioxidantes/metabolismo , Monosacáridos
7.
Environ Sci Technol ; 58(16): 7186-7195, 2024 Apr 23.
Artículo en Inglés | MEDLINE | ID: mdl-38598770

RESUMEN

Remediation of large and dilute plumes of groundwater contaminated by oxidized pollutants such as chromate is a common and difficult challenge. Herein, we show that in situ formation of FeS nanoparticles (using dissolved Fe(II), S(-II), and natural organic matter as a nucleating template) results in uniform coating of aquifer material to create a regenerable reactive zone that mitigates Cr(VI) migration. Flow-through columns packed with quartz sand are amended first with an Fe2+ solution and then with a HS- solution to form a nano-FeS coating on the sand, which does not hinder permeability. This nano-FeS coating effectively reduces and immobilizes Cr(VI), forming Fe(III)-Cr(III) coprecipitates with negligible detachment from the sand grains. Preconditioning the sand with humic or fulvic acid (used as model natural organic matter (NOM)) further enhances Cr(VI) sequestration, as NOM provides additional binding sites of Fe2+ and mediates both nucleation and growth of FeS nanoparticles, as verified with spectroscopic and microscopic evidence. Reactivity can be easily replenished by repeating the procedures used to form the reactive coating. These findings demonstrate that such enhancement of attenuation capacity can be an effective option to mitigate Cr(VI) plume migration and exposure, particularly when tackling contaminant rebound post source remediation.


Asunto(s)
Cromo , Agua Subterránea , Oxidación-Reducción , Contaminantes Químicos del Agua , Agua Subterránea/química , Cromo/química , Contaminantes Químicos del Agua/química , Nanopartículas/química , Restauración y Remediación Ambiental/métodos , Sustancias Húmicas , Compuestos Ferrosos/química , Benzopiranos/química
8.
BMC Plant Biol ; 24(1): 241, 2024 Apr 04.
Artículo en Inglés | MEDLINE | ID: mdl-38570771

RESUMEN

BACKGROUND: The global growth of pistachio production has prompted exploration into sustainable agricultural practices, on the application of humic substances such as fulvic acid in enhancing the quality of horticultural crops. The present study was carried out in Qom province, Iran, on 20 years old pistachio (Pistacia vera L. cv. Kaleh-Ghoochi) trees and investigated the impact of foliar spraying of fulvic acid at varying concentrations (1.5, 3, and 4.5 g L- 1) on the antioxidant and quality properties of pistachio. The different concentrations of fulvic acid were applied at two key stages: at the initiation of pistachio kernel formation (late June) and the development stage of pistachio kernel (late August), as well as at both time points. Following harvest at the horticulturally mature phase, various parameters, including total phenols, flavonoids, soluble proteins, soluble carbohydrate content, antioxidant capacity, and antioxidant enzyme activity, were assessed. RESULTS: Results indicated that foliar application of fulvic acid, particularly at 1.5 g L- 1 during both late June and August, effectively increased phenolic compounds (31.8%) and flavonoid content (24.53%). Additionally, this treatment also augmented antioxidant capacity and heightened the activity of catalase (CAT) (37.56%), ascorbate peroxidase (APX) (63.86%), and superoxide dismutase (SOD) (76.45%). Conversely, peroxidase (POX) (41.54%) activity was reduced in fulvic acid-treated nuts compared with controls. Moreover, the content of chlorophyll (45%) and carotenoids (46.7%) was enhanced using this organic fertilizer. In terms of mineral elements, the increment was observed in zinc (Zn) (58.23%) and potassium (K) (28.12%) amounts in treated nuts. Additionally, foliar application of fulvic acid led to elevated levels of soluble carbohydrates and proteins in treated nuts. CONCLUSIONS: In the present study, application of fulvic acid resulted in enhancement of antioxidant activity and quality traits of pistachio nut through an increase in total phenol, flavonoids, chlorophyll, carotenoids, K, Zn, and also activity of antioxidant enzymes. Therefore, use of fulvic acid emerges as a promising strategy to enhance the quality and nutritional attributes of pistachios, contributing to sustainable agricultural practices and improved crop outcomes.


Asunto(s)
Antioxidantes , Benzopiranos , Pistacia , Antioxidantes/análisis , Flavonoides/análisis , Fenoles , Carotenoides , Valor Nutritivo , Clorofila
9.
Nat Commun ; 15(1): 3539, 2024 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-38670975

RESUMEN

Bergenin, a rare C-glycoside of 4-O-methyl gallic acid with pharmacological properties of antitussive and expectorant, is widely used in clinics to treat chronic tracheitis in China. However, its low abundance in nature and structural specificity hampers the accessibility through traditional crop-based manufacturing or chemical synthesis. In the present work, we elucidate the biosynthetic pathway of bergenin in Ardisia japonica by identifying the highly regio- and/or stereoselective 2-C-glycosyltransferases and 4-O-methyltransferases. Then, in Escherichia coli, we reconstruct the de novo biosynthetic pathway of 4-O-methyl gallic acid 2-C-ß-D-glycoside, which is the direct precursor of bergenin and is conveniently esterified into bergenin by in situ acid treatment. Moreover, further metabolic engineering improves the production of bergenin to 1.41 g L-1 in a 3-L bioreactor. Our work provides a foundation for sustainable supply of bergenin and alleviates its resource shortage via a synthetic biology approach.


Asunto(s)
Benzopiranos , Vías Biosintéticas , Escherichia coli , Ingeniería Metabólica , Benzopiranos/metabolismo , Benzopiranos/química , Ingeniería Metabólica/métodos , Escherichia coli/metabolismo , Escherichia coli/genética , Glicosiltransferasas/metabolismo , Metiltransferasas/metabolismo , Ácido Gálico/metabolismo , Ácido Gálico/química , Reactores Biológicos , Glicósidos/biosíntesis , Glicósidos/metabolismo , Glicósidos/química
10.
Int J Mol Sci ; 25(8)2024 Apr 13.
Artículo en Inglés | MEDLINE | ID: mdl-38673904

RESUMEN

Chagas disease is one of the world's neglected tropical diseases, caused by the human pathogenic protozoan parasite Trypanosoma cruzi. There is currently a lack of effective and tolerable clinically available therapeutics to treat this life-threatening illness and the discovery of modern alternative options is an urgent matter. T. cruzi glucokinase (TcGlcK) is a potential drug target because its product, d-glucose-6-phosphate, serves as a key metabolite in the pentose phosphate pathway, glycolysis, and gluconeogenesis. In 2019, we identified a novel cluster of TcGlcK inhibitors that also exhibited anti-T. cruzi efficacy called the 3-nitro-2-phenyl-2H-chromene analogues. This was achieved by performing a target-based high-throughput screening (HTS) campaign of 13,040 compounds. The selection criteria were based on first determining which compounds strongly inhibited TcGlcK in a primary screen, followed by establishing on-target confirmed hits from a confirmatory assay. Compounds that exhibited notable in vitro trypanocidal activity over the T. cruzi infective form (trypomastigotes and intracellular amastigotes) co-cultured in NIH-3T3 mammalian host cells, as well as having revealed low NIH-3T3 cytotoxicity, were further considered. Compounds GLK2-003 and GLK2-004 were determined to inhibit TcGlcK quite well with IC50 values of 6.1 µM and 4.8 µM, respectively. Illuminated by these findings, we herein screened a small compound library consisting of thirteen commercially available 3-nitro-2-phenyl-2H-chromene analogues, two of which were GLK2-003 and GLK2-004 (compounds 1 and 9, respectively). Twelve of these compounds had a one-point change from the chemical structure of GLK2-003. The analogues were run through a similar primary screening and confirmatory assay protocol to our previous HTS campaign. Subsequently, three in vitro biological assays were performed where compounds were screened against (a) T. cruzi (Tulahuen strain) infective form co-cultured within NIH-3T3 cells, (b) T. brucei brucei (427 strain) bloodstream form, and (c) NIH-3T3 host cells alone. We report on the TcGlcK inhibitor constant determinations, mode of enzyme inhibition, in vitro antitrypanosomal IC50 determinations, and an assessment of structure-activity relationships. Our results reveal that the 3-nitro-2-phenyl-2H-chromene scaffold holds promise and can be further optimized for both Chagas disease and human African trypanosomiasis early-stage drug discovery research.


Asunto(s)
Benzopiranos , Glucoquinasa , Tripanocidas , Trypanosoma cruzi , Trypanosoma cruzi/efectos de los fármacos , Trypanosoma cruzi/enzimología , Tripanocidas/farmacología , Tripanocidas/química , Animales , Ratones , Benzopiranos/farmacología , Benzopiranos/química , Glucoquinasa/metabolismo , Glucoquinasa/antagonistas & inhibidores , Ensayos Analíticos de Alto Rendimiento , Enfermedad de Chagas/tratamiento farmacológico , Enfermedad de Chagas/parasitología , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/química , Células 3T3 NIH , Descubrimiento de Drogas/métodos , Humanos , Simulación del Acoplamiento Molecular , Relación Estructura-Actividad
11.
Medicina (Kaunas) ; 60(4)2024 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-38674192

RESUMEN

Background and Objective: Sapropel, a biologically active sedimentary deposit, is high in organic matter and minerals and has been shown to offer health benefits. Its constituents, humic acid (HA) and fulvic acid (FA), have been found to have some therapeutic applications. The aim of this study was to determine the potential therapeutically significant properties of freshwater sapropel extracts: their polyacid content, antioxidative (AO) status, and biological activity in cell culture. Materials and Methods: Freshwater lakes from the southeast region of Latvia were investigated layer by layer. The total organic carbon (TOC) was determined through combustion using the catalytic oxidation method, HA and FA were measured via acid perspiration, and the total polyphenol content (TPC) and total antioxidant status (TAS) was analysed spectrophotometrically. Sapropel extracts' regenerative abilities were tested in vitro using a Cell-IQ real-time monitoring system on mouse BALB/c 3T3 fibroblasts and human keratinocyte HaCaT cell lines. Cytotoxicity was measured through neutral red uptake assessment as a concentration-dependent reduction in the uptake of neutral red dye relative to a vehicle control or untreated cells. Results: The highest AO activity was observed in sapropel extracts with elevated concentrations of HA and TPC from Audzelu Lake (1.08 ± 0.03 mmol/L), and the lowest activity was found in extracts from Ivusku Lake (0.31 ± 0.01 mmol/L). Correspondingly, the concentrations of HA in Audzelu and Ivusku Lakes were recorded as 45.2 and 27.4 mg/g, respectively. High concentrations of HA promoted in vitro cell growth upon short-term exposure (up to 6 h). Conclusions: The results show that high TPC correlates with AO status and sapropel extracts with higher concentrations of HA exhibit greater AO activity and promote in vitro cell growth, suggesting a perspective use for short-term topical therapeutic skin applications. However, higher concentrations over longer durations showed cytotoxic effects, indicating the need for further investigation.


Asunto(s)
Antioxidantes , Animales , Antioxidantes/farmacología , Antioxidantes/análisis , Antioxidantes/uso terapéutico , Ratones , Humanos , Cuidados de la Piel/métodos , Sustancias Húmicas/análisis , Benzopiranos/análisis , Benzopiranos/farmacología , Benzopiranos/uso terapéutico , Agua Dulce/análisis , Técnicas In Vitro , Células HaCaT
12.
Environ Sci Technol ; 58(17): 7617-7627, 2024 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-38632682

RESUMEN

Commercial chemicals, such as synthetic musks, are of global concern, but data on their occurrence and spatial distribution in aquatic environments of large scale are scarce. Two sampling campaigns were conducted in the present study to measure freely dissolved synthetic musks in freshwaters across China using passive samplers, along with biological coexposure at selected sites. Polycyclic musks (PCMs) dominated synthetic musks, with a detection frequency of 95%. Higher concentrations of PCMs were observed in densely populated Mid, East, and South China compared to less populated regions, indicating the significance of anthropogenic activities for synthetic musks in water. The concentration ratios of galaxolide (HHCB)/tonalide (AHTN) were significantly higher in low-latitude areas than in high-latitude areas from June to September, suggesting that solar radiation played an important role in the degradation of HHCB/AHTN. Significant correlations were found between dissolved concentrations of HHCB and AHTN and their lipid-normalized concentrations in coexposed fish and clam. The estimated hazard quotients for HHCB and AHTN in freshwater fish consumed by humans were less than 0.01 at all sampling sites except the Yangtze River Basin. These results help to understand the environmental fate and ecological risks of synthetic musks on a large geographical scale.


Asunto(s)
Agua Dulce , Contaminantes Químicos del Agua , China , Contaminantes Químicos del Agua/análisis , Agua Dulce/química , Monitoreo del Ambiente , Bioacumulación , Benzopiranos , Animales , Tetrahidronaftalenos/análisis , Peces/metabolismo , Ácidos Grasos Monoinsaturados
13.
Water Res ; 256: 121603, 2024 Jun 01.
Artículo en Inglés | MEDLINE | ID: mdl-38631242

RESUMEN

Fulvic acid, prevalent in humus derived from the anaerobic digestion of kitchen wastewater, is crucial in organic matter transformation. However, its effects and underlying mechanisms remain unclear. In this study, the fate of anaerobic digestion of artificial and kitchen wastewater with different fulvic acid contents was investigated. The results showed that 125 mg/L fulvic acid resulted in a 64.02 and 51.72 % increase in methane production in synthetic and kitchen wastewater, respectively. Fulvic acid acted as an electron mediator and increased substrate oxidation by boosting NAD and ATP levels, thereby increasing microbial metabolic rates and ensuring an adequate substrate for methane generation. Isotope analysis suggested that fulvic acid boosts the conversion of volatile fatty acids to methane via the interspecies electron transfer pathway. Gene expression analysis revealed that cytochrome c, FAD, and other electron transport coenzymes were upregulated by fulvic acid, thereby enhancing substrate utilisation and biogas quality. Fulvic acid presented a dual stimulatory and inhibitory effect on anaerobic digestion, with concentrations over 125 mg/L diminishing its positive impact. This dual effect may stem from the properties and concentrations of fulvic acid. This study revealed the effect mechanism of fulvic acid and provided insights into the humus performance in anaerobic digestion.


Asunto(s)
Benzopiranos , Aguas Residuales , Aguas Residuales/química , Anaerobiosis , Eliminación de Residuos Líquidos , Metano/metabolismo , Reactores Biológicos
14.
Org Biomol Chem ; 22(17): 3459-3467, 2024 05 01.
Artículo en Inglés | MEDLINE | ID: mdl-38597668

RESUMEN

A water mediated three-component reaction of isatin, 4-aminocoumarin, and 1,3-cyclodicarbonyl compounds is reported for the synthesis of spiro[chromeno[4,3-b]cyclopenta[e]pyridine-7,3'-indoline]trione and the spiro[chromeno[4,3-b]quinoline 7,3'-indoline]trione. Up to 27 different spirooxindole derivatives were synthesized by this method. The bioactivity of these spirooxindole derivatives was evaluated and they were found to show antifungal activity against Cercospora arachidicola, Physalospora piricola, Rhizoctonia cerealis, and Fusarium moniliforme.


Asunto(s)
Antifúngicos , Benzopiranos , Indoles , Nitrilos , Compuestos de Espiro , Agua , Antifúngicos/farmacología , Antifúngicos/síntesis química , Antifúngicos/química , Compuestos de Espiro/farmacología , Compuestos de Espiro/química , Compuestos de Espiro/síntesis química , Agua/química , Indoles/química , Indoles/farmacología , Indoles/síntesis química , Pruebas de Sensibilidad Microbiana , Oxindoles/farmacología , Oxindoles/síntesis química , Oxindoles/química , Estructura Molecular , Relación Estructura-Actividad , Fusarium/efectos de los fármacos
15.
Bioresour Technol ; 400: 130703, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38631654

RESUMEN

Improving the humification of compost through a synergistic approach of biotic and abiotic methods is of great significance. This study employed a composite reagent, comprising Fenton-like agents and effective microorganisms (EM) to improve humification. This composite reagent increased humic-acid production by 37.44 %, reaching 39.82 g kg-1, surpassing the control group. The composite reagent synergistically promoted micromolecular fulvic acid and large humic acid production. Collaborative mechanism suggests that Fenton-like agents contributed to bulk residue decomposition and stimulated the evolution of microbial communities, whereas EMs promoted highly aromatic substance synthesis and adjusted the microbial community structure. Sequencing analysis indicates the Fenton-like agent initiated compost decomposition by Firmicutes, and EM reduced the abundance of Virgibacillus, Lentibacillus, and Alcanivorax. Applied as an organic fertilizer in Brassica chinensis L. plantations, the composite reagent considerably improved growth and photosynthetic pigment content. This composite reagent with biotic and abiotic components provides a learnable method for promoting humification.


Asunto(s)
Benzopiranos , Compostaje , Sustancias Húmicas , Peróxido de Hidrógeno , Hierro , Compostaje/métodos , Hierro/química , Hierro/farmacología , Peróxido de Hidrógeno/farmacología , Brassica , Microbiología del Suelo , Suelo/química , Bacterias , Fertilizantes
16.
Int J Biol Macromol ; 266(Pt 2): 131360, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38580017

RESUMEN

A humic acid-gelatin (HA-Gel) hydrogel, a gallic acid-xanthan gum (GA-XG) hydrogel, a HA-Gel/GA-XG hydrogel, and superabsorbent polymer (SAP) of HA-Gel/GA-XG/polyacrylamide (PAM) hydrogel were synthesized using electron beam irradiation method. The capability of synthesized hydrogels in loading and controlled release of fulvic acid (FA) was studied. The chemical and physical structure of sorbents was confirmed by various analyses. The effect of irradiation dose on mechanical properties, gel percentage, swelling, and absorbency under load (AUL) of the sorbents was investigated. By changing the hydrogel structures into the SAP form, its swelling capacity was increased from 37 to 320 g/g. Both hybrid hydrogel and SAP were reusable for up to 7 cycles. The maximum fertilizer loading capacities for SAP and hybrid hydrogel were 402.1 and, 175.5 mg g-1, respectively. In comparison to hydrogels, the SAP showed a slower FA-release performance. Thus, in soil media, 86 % of FA was released in 15-20 days from the hybrid hydrogel while with the SAP, 81 % of FA was released in 30-35 days. The significant improvement in the growth of fodder corn treated with FA-loaded SAP in the greenhouse media in comparison to the control groups showed the effective performance of the designed SAP, favoring its practical applications.


Asunto(s)
Benzopiranos , Gelatina , Hidrogeles , Polisacáridos Bacterianos , Zea mays , Hidrogeles/química , Benzopiranos/química , Polisacáridos Bacterianos/química , Gelatina/química , Zea mays/química , Preparaciones de Acción Retardada/química , Electrones , Polímeros/química , Fertilizantes , Ácido Gálico/química , Sustancias Húmicas
17.
Bioorg Med Chem Lett ; 106: 129770, 2024 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-38677560

RESUMEN

We have previously reported the total synthesis and structure-activity relationships (SAR) of 2-prenylated benzopyrans with PPAR agonist activity. Herein, we have described the synthesis and PPAR activity of 2-prenylated benzopyrans and 2-prenylated quinolines. The benzopyran nucleus was generated via enamine-catalyzed Kabbe condensation, and the quinoline nucleus via Friedländer condensation. Results demonstrated that both benzopyran (5a) and quinoline (4b) derivatives bearing a γ,δ-unsaturated ester displayed a pan-PPAR agonism. They were full PPARα agonists, but showed different preferences for PPARγ and PPARß/δ activation. It was noteworthy that quinoline 4b displayed full hPPARα activation (2-fold than WY-14,643), weak PPARß/δ and partial PPARγ activation. In addition, quinoline 4b showed anti-inflammatory effects on macrophages by reducing LPS-induced expression of both MCP-1 and IL-6. Therefore, 4b emerges as a first-in-class promising hit compound for the development of potential therapeutics aimed at treating metabolic syndrome, metabolic dysfunction-associated fatty liver disease (MAFLD), and its associated cardiovascular comorbidities.


Asunto(s)
Síndrome Metabólico , Quinolinas , Síndrome Metabólico/tratamiento farmacológico , Síndrome Metabólico/metabolismo , Quinolinas/química , Quinolinas/farmacología , Quinolinas/síntesis química , Relación Estructura-Actividad , Humanos , Receptores Activados del Proliferador del Peroxisoma/metabolismo , Receptores Activados del Proliferador del Peroxisoma/agonistas , Estructura Molecular , Lipopolisacáridos/farmacología , Lipopolisacáridos/antagonistas & inhibidores , Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Antiinflamatorios/química , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Relación Dosis-Respuesta a Droga , Benzopiranos/farmacología , Benzopiranos/síntesis química , Benzopiranos/química , Animales , Ratones
18.
World J Surg ; 48(5): 1177-1182, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38498009

RESUMEN

BACKGROUND: We evaluated the effectiveness of Ormeloxifene (Centchroman) on regression of Fibroadenoma in a double-blind randomized controlled trial. METHODS: Patients with biopsy proven Fibroadenoma were enrolled between March 2023 and October 2023 and divided in two arms- Ormeloxifene group and Placebo group. Effectiveness of the treatment was evaluated using USG. No residual mass was defined as complete regression and more than 30% decrease in size was considered as partial regression. RESULTS: A total of 130 consecutive patients with Fibroadenoma were randomized to Ormeloxifene group (n = 65) and Placebo Group (n = 65). Complete regression was observed in 9% (6/65) patients in Ormeloxifene group and 10.8% (7/65) in Placebo Group at the end of 12 weeks (p = 0.49). Twenty one patients taking Ormeloxifene reported adverse events as compared to none in the other group. CONCLUSION: In our study Ormeloxifene was not found to be effective in treatment of fibroadenoma and had concerning side effects.


Asunto(s)
Neoplasias de la Mama , Centcromano , Fibroadenoma , Humanos , Femenino , Fibroadenoma/tratamiento farmacológico , Fibroadenoma/patología , Método Doble Ciego , Adulto , Resultado del Tratamiento , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Centcromano/uso terapéutico , Persona de Mediana Edad , Adulto Joven , Benzopiranos
19.
Environ Sci Pollut Res Int ; 31(18): 27203-27220, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38507164

RESUMEN

Humified organic matter has been shown to decrease Pb toxicity in plants. However, there are still gaps in our understanding of the mechanism by which this phenomenon occurs. In this study, we aimed to assess the ability of humic substances (HSs), humic acids (HAs), and fulvic acids (FAs) to enhance defense mechanisms in rice plants under lead (Pb)-stressed conditions. HS fractions were isolated from vermicompost using the chemical fractionation methodology established by the International Humic Substances Society. These fractions were characterized by solid-state NMR and FTIR. Chemometric analysis was used to compare humic structures and correlate them with bioactivity. Three treatments were tested to evaluate the protective effect of humic fractions on rice plants. The first experiment involved the application of humic fractions along with Pb. The second comprised pretreatment with humic fractions followed by subsequent exposure to Pb stress. The third experiment involved Pb stress and subsequent treatment with humic fractions. The root morphology and components of the antioxidative defense system were evaluated and quantified. The results showed that HS + Pb, HA + Pb, and FA + Pb treatment preserved root growth and reduced the levels of O2- and malondialdehyde (MDA) in the roots by up to 5% and 2%, respectively. Pretreatment of the plants with humic fractions promoted the maintenance of root growth and reduced the contents of O2-, H2O2, and MDA by up to 48%, 22%, and 20%, respectively. Combined application of humic fractions and Pb reduced the Pb content in plant tissues by up to 60%, while pretreatment reduced it by up to 80%. The protective capacity of humic fractions is related to the presence of peptides, lignin, and carbohydrate fragments in their molecular structures. These results suggest that products could be developed that can mitigate the adverse effects of heavy metals on agricultural crops.


Asunto(s)
Benzopiranos , Sustancias Húmicas , Plomo , Oryza , Contaminantes del Suelo , Estructura Molecular , Contaminación Ambiental
20.
Environ Sci Technol ; 58(12): 5524-5533, 2024 Mar 26.
Artículo en Inglés | MEDLINE | ID: mdl-38466636

RESUMEN

The high environmental concentrations, persistence, and toxicity of synthetic musk compounds (SMCs) necessitate a better grasp of their fate in wastewater treatment plants (WWTPs). To investigate the importance of WWTPs as pathways of SMCs to the environment, air and wastewater samples were collected at four WWTPs in Ontario, Canada. Polycyclic musks (PCMs) were present at higher concentrations than nitro musks (NMs) and macrocyclic musks (MCMs). Three PCMs [galaxolide (HHCB), tonalide (AHTN), and iso-E super (OTNE)] were the most abundant compounds (0.30-680 ng/m3 in air, 0.40-15 µg/L in influent, and 0.007-6.0 µg/L in effluent). Analyses of multiyear data suggest that risk management measures put in place have been effective in reducing the release of many SMCs into the environment. The highest removal efficiency, up to almost 100% of some SMCs, was observed for the plant with the longest solid retention time. A fugacity-based model was established to simulate the transport and fate of SMCs in the WWTP, and good agreement was obtained between the measured and modeled values. These findings indicate that the levels of certain SMCs discharged into the atmospheric and aquatic environments were substantial, potentially resulting in exposure to both humans and wildlife.


Asunto(s)
Ácidos Grasos Monoinsaturados , Contaminantes Químicos del Agua , Purificación del Agua , Humanos , Contaminantes Químicos del Agua/análisis , Aguas Residuales , Ontario , Benzopiranos/análisis
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